Meyer D, Schaefer M, Bonnemain B
Recherche Chimique, Laboratoire Guerbet, Aulnay-sous-Bois, France.
Invest Radiol. 1988 Sep;23 Suppl 1:S232-5. doi: 10.1097/00004424-198809001-00048.
The complex (Gd-DOTA) meglumine has recently been used as an MRI contrast agent in humans. Due to its particularly interesting physicochemical properties, the risk of in vivo dissociation of the complex is reduced. Indeed, as a result of the macrocyclic nature of the DOTA ligand, Gd-DOTA appears very stable, demonstrating a calculated conditional stability constant of 10(22.19) at pH = 7. Other characteristics making Gd-DOTA a positively attractive compound include slow dissociation kinetics inherent in the rigidity of the macrocycle and marked specific affinity of DOTA for gadolinium in comparison with other endogenous ions. Finally, although the relaxivity R1 of Gd-DOTA at 20 MHz appears similar to that of Gd-DTPA, Gd-DOTA demonstrates higher paramagnetic efficacy at low field strength due to greater symmetry of the complex. Such promising properties open up wide prospects for the use of Gd-DOTA in MRI.
钆喷酸葡胺（Gd-DOTA）复合物最近已被用作人体磁共振成像（MRI）造影剂。由于其特别有趣的物理化学性质，该复合物在体内解离的风险降低。事实上，由于DOTA配体的大环性质，钆喷酸葡胺显得非常稳定，在pH = 7时计算得出的条件稳定常数为10(22.19)。使钆喷酸葡胺成为极具吸引力的化合物的其他特性包括大环刚性所固有的缓慢解离动力学，以及与其他内源性离子相比，DOTA对钆有显著的特异性亲和力。最后，尽管钆喷酸葡胺在20 MHz时的弛豫率R1似乎与钆二乙三胺五乙酸（Gd-DTPA）相似，但由于该复合物具有更高的对称性，钆喷酸葡胺在低场强下表现出更高的顺磁效能。这些有前景的特性为钆喷酸葡胺在MRI中的应用开辟了广阔前景。
